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Helios degrader ALV1

Chemical Structure : Helios degrader ALV1

CAS No.: 2438124-79-7

Helios degrader ALV1 (ALV-03-112-01)

Catalog No.: PC-38302Not For Human Use, Lab Use Only.

Helios degrader ALV1 (ALV-03-112-01) is a small molecule degrader of the zinc-finger transcription factor Helios with IC50 of 0.55 uM in CRBN-binding TR-FRET assay.

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Biological Activity

Helios degrader ALV1 (ALV-03-112-01) is a small molecule degrader of the zinc-finger transcription factor Helios with IC50 of 0.55 uM in CRBN-binding TR-FRET assay.
ALV1 recruit the E3 ubiquitin ligase substrate receptor cereblon to Helios.
ALV1 bound CRBN in vitro with greater potency than lenalidomide but less than CC-885.
ALV1 also induced CRBN-Helios dimerization in the TR-FRET assay, with greater activity than either CC-885. ALV1 degraded both Ikaros and Helios.

Physicochemical Properties

M.Wt 494.932
Formula C25H23ClN4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-chloro-4-methylphenyl)-3-(3-((1-(2,6-dioxopiperidin-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)amino)phenyl)propanamide

References

1. Eric S Wang, et al. Nat Chem Biol. 2021 Jun;17(6):711-717.

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